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KMID : 0369819940240030145
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Jorunal of Korean Pharmaceutical Sciences
1994 Volume.24 No. 3 p.145 ~ p.153
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Effects of Suppository Bases and Additives on Rectal Absorption of Ibuprofen Lysinate
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전홍렬/Jeon HR
박동우/이승목/이정우/최영욱/Park DW/Lee SM/Yi JW/Choi YW
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Abstract
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Ibuprofen is an effective non-steroidal anti-inflammatory drug (NSAID), but it has several limitations in clinical application because of low solubility in water and gastrointestinal irritation. A water-soluble salt of ibuprofen, ibuprofen Iysinate, has been synthesized to overcome these shortcomings, and it was formulated as suppository for rectal administration. Witepsol and polyethylene glycols were employed as suppository bases for either ibuprofen or ibuprofen Iysinate, in order to compare the bioavailability in rabbits. The plasma concentrations of ibuprofen were assayed by HPLC after a rectal administration of ibuprofen and ibuprofen Iysinate, respectively. In addition to the comparison of two suppository bases, the other factors which affect on rectal absorption were also evaluated, especially in the point of not only particle size and shape of ibuprofen Iysinate but also effects of additives such as stearic acid, cetyl alcohol and capric acid. And pharmacokinetic parameters such as AUC, Cmax, and Tmax were also compared. In conclusion, spray-dried ibuprofen Iysinate which was polyporous and spherical shape gave an increased absorption from the rectal formulations with Witepsol Hl5 and stearic acid.
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KEYWORD
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Ibuprofen, Ibuprofen Iysinate, Suppository bases, Additives, Rectal absorption, Relative bioavailability
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